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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
42 Results for "
dimethylation
" in MedChemExpress (MCE) Product Catalog:
Products (42)
42 Results for "dimethylation" in MCE Product Catalog:
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10 Publications Verification
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TP-064, a chemical probe, is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities .
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Infection Microorganisms Antibiotics Disease Research Antibacterial Disease Research Fields Other Antibiotics
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1 Cited Publications
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Natural Products Animals Marine natural products Other marine organisms Disease Research Fields Cancer
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1 Cited Publications
Cat. No.: HY-P1108
CAS No.: 681260-70-8
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1 Cited Publications
Cat. No.: HY-P1108A
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1 Cited Publications
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MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
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Cat. No.: HY-P10272
CAS No.: 1628323-80-7
Synonyms: PTG-300
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WIZ degrader 9 is an orally active molecular glue degrader of the WIZ transcription factor. As a molecular glue, WIZ degrader 9 recruits WIZ to the cereblon E3 ubiquitin ligase complex via its ZF7 domain, driving proteasome-dependent degradation of WIZ. WIZ degrader 9 induces hemoglobin production, reduces the level of H3K9 dimethylation across the whole genome and at the β-globin locus, upregulates the transcription of γ-globin and BGLT3, and increases the level of histone H3K9 acetylation in the promoter region of HBG1/2. WIZ degrader 9 effectively induces fetal hemoglobin production in both mice and cynomolgus monkeys. WIZ degrader 9 can be used for research on sickle cell disease .
Cat. No.: HY-159098
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dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease .
Cat. No.: HY-162308
CAS No.: 744260-15-9
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NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .
Cat. No.: HY-44062
CAS No.: 1350752-07-6
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G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
Cat. No.: HY-178825
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LD-110 is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer .
Cat. No.: HY-P10143
CAS No.: 99828-55-4
Synonyms: Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt
Cat. No.: HY-A0248AS
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Cat. No.: HY-101520A
Purity: 98.56%
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Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 TFA potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively .
Cat. No.: HY-172614
CAS No.: 313527-11-6
Synonyms: RK-552
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RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .
Cat. No.: HY-P10563
CAS No.: 2580150-96-3
Synonyms: BHV-1100
Cat. No.: HY-176036
CAS No.: 3070323-06-4
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MS1262 is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC50 of 19 nM and a Kd of 74 nM against G9a, and an IC50 of 6 nM and a Kd of 19 nM against GLP. MS1262 reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 reduces the risk of thrombus rupture. MS1262 can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer .
Cat. No.: HY-P3066
CAS No.: 77453-01-1
Synonyms: d(CH2)5Tyr(Et)VAVP
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
